2019 » Johns Hopkins Drug Discovery
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161. Vornov JJ, Peters D, Nedelcovych M, Hollinger K, Rais R, Slusher BS. “Looking for Drugs in All the Wrong Places: Use of GCPII Inhibitors Outside the Brain.”, Neurochem Res. 2019 Nov 20, [PubMed]

160. Leone RD, Zhao L, Englert JM, Sun IM, Oh MH, Sun IH, Arwood ML, Bettencourt IA, Patel CH, Wen J, Tam A, Blosser RL, Prchalova E, Alt J, Rais R, Slusher BS, Powell JD. “Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion.”, Science, 2019, Nov. 7 [PubMed]

159. Slack RD, Ku T, Cao J, Giancola J, Bonifazi A, Loland CJ, Gadiano A, Lam J, Rais R, Slusher BS, Coggiano M, Tanda G, Newman AH. “Structure-Activity Relationships for a series of bis(4-fluorophenyl)methyl)sulfinyl)alkyl alicyclic amines at the dopamine transporter: functionalizing the terminal nitrogen affects affinity, selectivity and metabolic stability.”J Med Chem, 2019, Oct 29 [PubMed]

158.  Shaik AB, Kumar V, Bonifazi A, Guerrero A, Cemaj S, Gadiano A, Lam J, Xi ZX, Rais R, Slusher BS, Newman AH. “Investigation of novel primary and secondary pharmacophores, and 3-substitution in the linking chain of a series of highly selective and bitopic dopamine D3 receptor antagonists and partial agonists.”, J Med Chem, 2019, Oct 24;62(20):9061-9077 [PubMed]

157.  Dash RP, Tichý T, Veeravalli V, Lam J, Alt J, Wu Y, Tenora L, Majer P, Slusher BS, Rais R. “Enhanced Oral Bioavailability of 2-(Phosphonomethyl)-pentanedioic Acid (2-PMPA) from its (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl (ODOL-Based Prodrugs.”, Mol Pharm, 2019, Oct 7;16(10):4292-4301  [PubMed]

156.  Prchalová E, Hin N, Thomas AG, Veeravalli V, Ng J, Alt J, Rais R, Rojas C, Li Z, Hihara H, Aoki M, Yoshizawa K, Nishioka T, Suzuki S, Kopajtic T, Chatrath S, Liu Q, Dong X, Slusher BS, Tsukamoto T.  “Discovery of Benzamidine-and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.”  J Med Chem, 2019, Sep 26;62(18):8631-8641 [PubMed]

155.  Hollinger KR, Smith MD, Kirby LA, Prchalova E, Alt J, Rais R, Calabresi PA, Slusher BS.  “Glutamine antagonism attenuates physical and cognitive deficits in a model of MS.”  Neurol Neuroimmunol Neuroinflamm., 2019 Aug 29;6(6) [PubMed]

154.  Hanaford AR, Alt J, Rais R, Wang SZ, Kaur H, Thorek DLJ, Eberhart CG, Slusher BS, Martin AM, Raabe EH., “Orally bioavailable glutamine antagonist prodrug JHU-083 penetrates mouse brain and suppresses the growth of MYC-driven medulloblastoma.” Transl Oncol, 2019, Jul 21;12(10):1314-1322  [PubMed]

153. Soomro I, Sun Y, Li Z, Diggs L, Hatzivassiliou G, Thomas AG, Rais R, Parker SJ, Slusher BS, Kimmelman AC, Somlo S, Skolnik EY. “Erratum.”, Nephrol Dial Transplant, 2019 May 20 [PubMed]

152. Wang SZ, Poore B, Alt J, Price A, Allen SJ, Hanaford AR, Kaur H, Orr BA, Slusher BS, Eberhart CG, Raabe EH, Rubens JA. “Unbiased Metabolic Profiling Predicts Sensitivity of High MYC-Expressing Atypical Teratoid/Rhabdoid Tumors to Glutamine Inhibition with 6-Diazo-5-Oxo-L-Norleucine.”  Clin Cancer Res, 2019, Oct 1;25(19):5925-5936 [PubMed]

151. Rojas C, Sala M, Thomas AG, Datta Chaudhuri A, Yoo SW, Li Z, Dash RP, Rais R, Haughey N, Nencka R, Slusher B., “A novel and potent brain penetrant inhibitor of extracellular vesicle release.”, Br J Pharmacol., 2019, Oct;176(19):3857-3870 [PubMed]

150. Battiti FO, Cemaj SL, Guerrero AM, Shaik AB, Lam J, Rais R, Slusher BS, Deschamps JR, Imler GH, Newman AH, Bonifazi A. “The significance of chirality in drug design and synthesis of bitopic ligands as D3 receptor (D3R) selective agonists.” J Med Chem., 2019, Jul 11;62(13):6287-6314 [PubMed]

149.  Udupa S, Nguyen S, Hoang G, Nguyen T, Quinones A, Pham K, Asaka R, Nguyen K, Elgogary A, Jung JG, Xu Q, Fu J, Thomas AG, Tsukamoto T, Hanes J, Slusher BS, Cooper AJL, Le A. “Upregulation of the Glutaminase II Pathway Contributes to Glutamate Production upon Glutaminase 1 Inhibition in Pancreatic Cancer.” Proteomics, 2019, June 24 [PubMed]

148.  Nedelcovych MT, Kim BH, Zhu X, Lovell LE, Manning AA, Kelschenbach J, Hadas E, Chao W, Prchalova E, Dash RP, Wu Y, Alt J, Thomas AG, Rais R, Kamiya A, Volsky DJ, Slusher BS. “ Glutamine Antagonist JHU083 Normalizes Aberrant Glutamate Production and Cognitive Deficits in the EcoHIV Murine Model of HIV-Associated Neurocognitive Disorders.” J of Neuroimmune Pharm, 2019, Sep;14(3):391-400[PubMed]

147.  Cuesta S, Restrepo-Lozano JM, Popescu C, He S, Reynolds LM, Israel S, Hernandez G, Rais R, Slusher BS, Flores C. “DCC-related developmental effects of abused- versus therapeutic-like amphetamine doses in adolescence. Addiction Biology, 2019 [PubMed]

146.  Jordan CJ, Humburg B, Rice M, Bi GH, You ZB, Shaik AB, Cao J, Bonifazi A, Gadiano A, Rais R, Slusher B, Newman AH, Xi ZX.  Neuropharmacology, 2019, Nov 1;158:107597[PubMed]

145.  Kim BH, Kelschenbach J, Borjabad A, Hadas E, He H, Potash MJ, Nedelcovych MT, Rais R, Haughey NJ, McArthur JC, Slusher BS, Volsky DJ.   “Intranasal insulin therapy reverses hippocampal dendritic injury and cognitive impairment in a model of HAND in Eco-HIV-infected mice.” AIDS, 2019, May 1;33(6):973-984[PubMed]

144.  Stepanek O, Hin N, Thomas AG, Dash RP, Alt J, Rais R, Rojas C, Slusher BS, Tsukamoto T.  “Neutral Sphingomyelinase 2 inhibitors based on the 4-(1H-imidazol-2-yl)-2,6-dialkoxyphenol scaffold.”  Eur J Med Chem, 2019, May 15;170:276-289. [PubMed]

143.  Tenora L, Alt J, Dash RP, Gadiano AJ, Novotna K, Veeravalli V, Lam J, Kirkpatrick QR, Lemberg KM, Majer P, Rais R, Slusher BS.  “Tumor-Targeted Delivery of 6-Diazo-5-oxo-I-norleucine (DON) Using Substituted Acetylated Lysine Prodrugs.”  J Med Chem, 2019, April 11;62(7):3524-3538  [PubMed]

142. Hollinger KR, Alt J, Rais R, Kaplin AI, Slusher BS.  “The NAAG’ing Concerns of Modeling Human Alzheimer’s Disease in Mice.”  J Alzheimer’s Dis, 2019, 68(3):939-945 [PubMed]

141.  Zhu X, Nedelcovych MT, Thomas AG, Hasegawa Y, Moreno-Megui A, Coomer W, Vohra V, Saito A, Perez G, Wu Y Alt J, Prchalova E, Tenora L, Majer P, Rais R, Rojas C, Slusher BS, Kamiya A. “Correction: JHU-083 selectivity blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.” Neuropsychopharmacology, 2019, May:44 (6):1178 [PubMed]

140. You ZB, Bi GH, Galaj E, Kumar V, Cao J, Gadiano A, Rais R, Slusher BS, Gardner EL, Xi ZX, Newman AH. “Dopamine D3R antagonist VK4-116 attenuates oxycodone self-administration and reinstatement without compromising its antiociceptive effects.” Neuropsychopharmacology, 2019, Jul;44(8):1415-1424. [PubMed]

139. Barinka C, Novakova Z, Hin N, Bim D, Ferraris DV, Duvall B, Kabarriti G, Tsukamoto R, Budesinsky M, Motlova L, Rojas C, Slusher BS, Kamiya A. “Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.” Bioorg Med Chem, 2019, Jan 15;27(2):255-264 [PubMed]

138.  Poore B, Yuan M, Arnold A, Price A, Alt J, Rubens JA, Slusher BS, Eberhart CG, Raabe EH. “Inhibition of mTORC1 in pediatric low-grad glioma depletes glutathione and therapeutically synergizes with carboplatin.”, NeuroOncol, 2019 Feb 14;21(2):252-263. [PubMed]

137.   Zhu X, Nedelcovych MT, Thomas AG, Hasegawa Y, Moreno-Megui A, Coomer W, Vohra V, Saito A, Perez G, Wu Y Alt J, Prchalova E, Tenora L, Majer P, Rais R, Rojas C, Slusher BS, Kamiya A. “JHU-083 selectivity blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.” Neuropsychopharmacology, 2019, Mar:44 (4):683-694 [PubMed]